Introduction to hypoglycemic drugs: Insulinotropic Agent (medicine)

Insulinotropic agents are alternate first-line hypoglycemic agents, which are available as sulfonylureas as well as non-sulfonylureas.

1. Sulphonylurea
These drugs are suitable for patients with type 2 diabetes who have certain insulin secretion function and normal liver and kidney function, and can be used alone or in combination with other hypoglycemic drugs to increase their hypoglycemic effect.

(i) Glibenclamide (Meprid, Ruiyunin, Disa, Epirubicin, Udalin)
This class of drugs is the second generation of sulfonylurea drugs, fast-acting, the efficacy in the human body can last 6-8 hours, especially effective in reducing postprandial hyperglycemia; due to its metabolites inactive and fast excretion, it is less likely to cause hypoglycemia than glibenclamide, suitable for elderly patients.

(II) Gliclazide (Damecon)
This class of drugs is the second generation of sulfonylurea drugs, its efficacy is more than 10 times stronger than the first generation of toluene sulfobutylurea; in addition, it also inhibits platelet adhesion and aggregation, which can effectively prevent microthrombosis, thus can prevent microangiopathy in type 2 diabetes mellitus. It is suitable for adult type 2 diabetes, type 2 diabetes with obesity or associated vascular pathology. Use with caution in the elderly and those with impaired renal function.

(III) Glibenclamide (euglycemic)
This class of drugs is the second generation of sulfonylureas, it is the strongest of all sulfonylureas glucose-lowering effect, 200-500 times more than tolbutamide, its effect can last for 24 hours. It can be used for mild to moderate non-INSULIN-dependent type 2 diabetes, but it is prone to hypoglycemia and should be used with caution in the elderly and those with renal insufficiency.

(iv) Glipozide (Glucuronide)

20 times more potent than first-generation methylprednisolone, more easily absorbed and less likely to cause hypoglycemia than glibenclamide; its effect lasts for 24 hours. It can be used for non-insulin-dependent type 2 diabetes.

(v) Glimepiride (Amory)

It is the third generation of oral sulfonylurea drugs, its mechanism of action is the same as other sulfonylureas, but it can increase the cardiac glucose uptake through a pathway unrelated to insulin, so it affects less cardiovascular system than other oral hypoglycemic drugs; its in vivo half-life can be as long as 9 hours, only need to be taken orally once a day. It is indicated for non-insulin-dependent type 2 diabetes.

(vi) Glycopyrrolizidine (Glucophage)

The second generation oral sulfonylurea hypoglycemic drug is a highly active pro-insulin β-cell agent, which binds to the specific receptor on the pancreatic β-cell membrane and can induce the production of appropriate amount of insulin to reduce blood glucose concentration. The highest blood concentration of this product is reached 2~2.5 hours after oral administration, and it is quickly and completely absorbed. The plasma half-life is 1.5 hours, and the metabolism is complete; its metabolites have no hypoglycemic effect; most of the metabolites are excreted through the biliary digestive system. It is suitable for mild or moderate non-insulin-dependent type 2 diabetes mellitus in which the therapeutic effect of diet alone is not satisfactory, and the patient's pancreatic islet B cells have a certain function of insulin secretion, and there are no serious complications.

The above are the commonly used sulfonylurea glucose-lowering drugs, and the order of their glucose-lowering intensity from strong to weak is: glibenclamide>glibenclamide>gliquinolone>gliclazide.

2. Non-sulphonylureas (phenylethanoid derivatives as secretagogues)

 It stimulates the release of insulin from pancreatic B cells and restores physiological insulin secretion, effectively reducing fasting and postprandial hyperglycemia.

It was found that insulin secretion was restored to healthy control levels in the reglinex treatment group. Repaglinide also restores insulin
Pulsatile secretion of the hormone and to some extent improves insulin sensitivity. Commonly used drugs are Reglinex and naglinex. Repaglinide
Nai (Novolone): this drug does not cause severe hypoglycemia, does not cause liver damage, and is useful in patients with moderate liver and kidney damage.

The drug is also well tolerated, has fewer drug interactions, and is suitable for postprandial glycemic control.